Tanshinone I, also known as tanshinquinone I, has a chemical formula of 1,6-dimethyl-phenanthreno [1,2-b]furan-10,11-diketone and is extracted from the roots and stems of a Lamiaceae family plant, the Salvia miltiorrhiza Bge. Tanshinone I has various pharmacological effects and a wide range of clinical use. It can be used for the treatment of coronary heart disease, angina, myocardial infarction, viral myocarditis, cardiac arrhythmia, cerebral vascular disease, cerebral ischemia, cerebral thrombosis, cerebral infarction, hepatitis, tumor, hypertension and other diseases. Therefore, scientists have conducted a multitude of research on the following tanshinone derivatives.

Tanshinone I has poor solubility in water, and thus has low in vivo bioavailability. Therefore, scientists have attempted to modify the structure of tanshinone I in order to improve its water solubility and bioavailability so as to magnify the medicinal value of tanshinone I. (QIN Yinlin, Tanshinone I derivatives and applications thereof in pharmaceuticals, [P] CN 1837199A, 2006; QIN Yinlin, Tanshinone I derivatives and applications thereof in pharmaceuticals, [P] CN 1837200A, 2006; DU Zhiyun et al., Tanshinone derivatives and applications thereof in the preparation of a medicament for aldose reductase inhibitors, [P] CN 101012270A, 2007.)
Tanshinone I possesses certain antitumor effects. It is reported that, by observing the effects of tanshinone I on various indices of Hep G2 cells in in vitro and in vivo experiments, one can make an overall judgment whether it possesses anti-tumor effects. Results from the in vitro experiments indicate that tanshinone I can inhibit the proliferation of Hep G2 cells. In addition, results from the tumor inhibition experiments carried out on tumor-bearing nude mice indicate that tanshinone I can inhibit the tumor growth in the mice. That is, tanshinone I possesses antitumor effects in vivo as well. (ZHENG Guocan, L I Zhiying, Study on the inhibiting effect of Tanshinone I on HepG2 cell line in vitro, Modern Medical Journal, 2004, 32 (15): 296-298; ZHENG Guocan, L I Zhiying, Study on the anti-tumor effect and mechanism of tanshinone I, Journal of Practical Oncology, 2005, 20 (1): 33-35).
In addition, some studies have reported the effects of tanshinone I on the proliferation and apoptosis of SGC-7901 gastric adenocarcinoma cells in vitro. Experiments have found out that tanshinone I has significant inhibitory effect on the growth of the SGC-7901 human gastric adenocarcinoma cells cultured in vitro, and the inhibition of the cell growth is dependent on the concentration of tanshinone I within a certain range. (ZHOU Xiaoli et al., The effect of Tanshinone I on proliferation and apoptosis of human gastric adenocarcinoma cell line SGC-7901, Journal of Modern Oncology, 2011, 19 (3): 423-427.)
In spite of the multitude of studies on the structural modifications and bioactivity of tanshinone I, reports on the synthesis and application of antitumor tanshinone compounds with good water solubility, low toxicity and excellent bioactivity have not yet been seen.